Process for preparing heterocyclic compounds

摘要

The preparation of N-(heterocyclyl-methyl)-substituted cyclic cyanoimino-amidines (I) comprising alkylation of an N-unsubstituted analog is carried out in a protic solvent. Preparation of N-substituted cyclic cyanoamidines of formula (I) involves reacting an N-unsubstituted analog of formula (II) with an alkylating agent of formula Y-CHR1-M1 (III) in presence of a protic solvent and optionally a base. R1, R3 = H or alkyl; A = (CH2)2 or (CH2)3 (both optionally substituted by alkyl); X = O, S or CHR3; Y = optionally substituted 5- or 6-membered heterocyclic group containing at least two of O, S and N as heteroatoms; or optionally substituted 3- or 4-pyridyl; M1 = halo or OSO2M2; M2 = lower alkyl, aryl or OM3; M3 = lower alkyl or alkali metal.